Timolol - instructions for use, dose, side effects, contraindications

Composition:Composition per ml: active substance: timolol maleate (in terms of timolol) 2.5 mg or 5.0 mg; auxiliary substances: sodium hydrogen phosphate dodecahydrate, sodium dihydrogen phosphate dihydrate, sodium chloride, disodium edetate dihydrate, benzalkonium chloride, water for injection

Description:clear colorless liquid

Pharmacotherapeutic group:Antiglaucoma means β-blocker.

ATX: & nbsp

S.01.E.D. Beta-blockers

S.01.E.D.01 Timolol

Pharmacodynamics:A non-selective beta-adrenergic receptor blocker without sympathomimetic activity. With topical application lowers the intraocular pressure due to a decrease in the formation of watery moisture and a small increase in its outflow. Reducing intraocular pressure, does not affect the accommodation and the size of the pupil, so there is no deterioration of visual acuity and the quality of night vision does not decrease. The effect manifests itself 20 minutes after instillation, the maximum effect after 1-2 hours; the duration of the action is 24 hours.

Pharmacokinetics:

After the installation of eye drops in the moisture of the anterior chamber of the eye, the time to reach the maximum concentration is 1-2 hours.The active substance enters the systemic circulation by absorption through the conjunctiva, the mucous membranes of the nose and the lacrimal tract. The drug is metabolized by the isoenzyme CYP2D6. Excretion of metabolites by the kidneys. In newborns, the concentration of the active substance is significantly higher than its maximum concentration in adult plasma.

Indications:

Eye hypertension, open-angle glaucoma, secondary glaucoma (uveal, aphakic, post-traumatic);

As an auxiliary drug: zakratougolnaya glaucoma (in combination with miotikami), congenital glaucoma (with ineffectiveness of other therapeutic measures), acute increase in intraocular pressure.

Contraindications:

Contraindications

Hypersensitivity, dystrophic processes in the cornea, bronchial asthma (including in history), severe chronic obstructive pulmonary disease, sinus bradycardia, atrioventricular blockade of II-III degree, decompensated chronic heart failure, cardiogenic shock, children under 18 years old, lactation period.

Carefully:

Sinoatrial blockade of MI degree, arterial hypotension, atrophic rhinitis,pulmonary insufficiency, severe cerebrovascular insufficiency, diabetes mellitus, hypoglycemia, thyrotoxicosis, myasthenia gravis, simultaneous administration of other beta-adrenoblockers, pheochromocytoma, peripheral circulation disorders (including Raynaud's syndrome), pregnancy.

With caution apply simultaneously with antihypertensive drugs, other beta-blockers, insulin or oral hypoglycemic drugs, glucocorticosteroid, psychoactive drugs, as well as drugs whose effect is associated with increased adrenaline release.

Pregnancy and lactation:

The use of the drug during pregnancy is possible only if the intended benefit to the mother exceeds the potential risk to the fetus.

If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped.

If the drug was used immediately before delivery, the newborns should be carefully monitored for several days after birth.

Dosing and Administration:

Adults instill in the conjunctival sac 1 drop 0.25% solution 2 times a day, with insufficient efficiency - 1 drop of 0.5% solution 2 times a day. Evaluation of the hypotensive effect should be performed after 2 weeks of regular use.

Recommendations for the use of vials with droppers: Before using the drug, remove the aluminum cap from the bottle, remove the rubber stopper and close the bottle with a dropper, previously released from the package. Then remove the cap from the cap-dropper, turn the bottle, drip the required number of drops of the drug. After applying the bottle, return to the vertical position and put the cap on the lid-dropper.

Recommendations for the use of a tube-dropper (t / k): remove the protective cap, cut off the membrane of the neck of the body with scissors, without damaging the threaded part. Turn the body t / k with the drug throat down and gently move the body t / k, using it as a pipette. After applying the recommended dose of the doctor or specified in the instructions for use of the drug dose, the body t / k turn the threaded part up and screw the protective cap.

Side effects:

Local reactions: conjunctival irritation - conjunctival hyperemia, lacrimation or tearing, photophobia, corneal epithelial edema, burning and itching in the eyes, hyperemia of the eyelid skin, short-term visual acuity; blepharitis, conjunctivitis, keratitis, with prolonged use, it is possible to develop a surface point keratopathy (decrease the transparency of the cornea) and decrease the sensitivity of the cornea, it is possible ptosis, rarely - diplopia.

Systemic reactions: paresthesia, rhinitis, nasal congestion, epistaxis, lowering of arterial pressure, collapse, bradycardia, bradyarrhythmia, atrioventricular blockade, decreased myocardial contractility, worsening of manifestations of chronic heart failure; headache, dizziness, drowsiness, hallucinations, depression, myasthenia gravis, decreased potency; shortness of breath, bronchospasm, pulmonary insufficiency; nausea, vomiting, diarrhea, chest pain, ringing in the ears.

Allergic reactions (including urticaria).

Overdose:

Symptoms: it is possible to develop general-resorptive effects typical for beta-adrenoblockers (dizziness, headache, arrhythmia, bradycardia, bronchospasm, nausea, vomiting).

Treatment: immediately flush eyes with water or 0.9% solution of sodium chloride, symptomatic therapy.

Interaction:

Epinephrine and pilocarpine increase the hypotensive effect of timolol. Simultaneous administration of eye drops containing epinephrine, can cause a dilated pupil (mydriasis).

Concomitant use with inhibitors of the isoenzyme CYP2D6 (amiodarone, quinidine, haloperidol, paroxetine, fluoxetine, citalopram, sertraline, terbinafine, ketoconazole, ritonavir, cimetidine) can provoke the appearance of symptoms of thymolol overdose, including severe bradycardia (up to a heart rate of less than 40 per min), in some cases - and deep lethargy.

Strengthens the action of muscle relaxants and general anesthetics (a few days before the general anesthesia with chloroform or diethyl ether or with the use of peripheral muscle relaxants it is necessary to stop the instillation of the drug).

Against the background of drug treatment, intravenous administration of verapamil, diltiazem (possibly suppressing atrioventricular conduction, development of bradycardia and lowering blood pressure) should be avoided.

Special instructions:

Control of effectiveness is recommended to be performed approximately 3-4 weeks after the start of therapy (not earlier than in 1-2 weeks). With prolonged use of timolol, the effect may be weakened.

Form release / dosage:

Eye drops 0.25% and 0.5%.

5 ml in bottles of glass, ukupostoppers rubber and обкатанwith aluminum caps. Bottle together with a dropper and instructionfor use in a pack of cardboard.

1 ml per tube-dropper.

2 tubes of IV drip along with the instructionsher use on the package in a pack of cardboard.

2 tubes are placed in the contourcell packaging from a polyvinyl chloride and aluminum foil printed lacquered.

1 circuit cell pack together with an instruction for use is placed in a pack of cardboard.

Packaging:

5 ml in bottles of glass, ukupostoppers rubber and обкатанwith aluminum caps. Bottle together with a dropper and instructionfor use in a pack of cardboard.

1 ml per tube-dropper.

2 tubes of IV drip along with the instructionsher use on the package in a pack of cardboard.

2 tubes are placed in the contourcell packaging from a polyvinyl chloride and aluminum foil printed lacquered.

1 circuit cell pack together with an instruction for use is placed in a pack of cardboard.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C. Do not freeze.

Shelf life:

2 years.

The bottle should be stored for 4 weeks after opening.

Do not use after the expiration date printed on the package. Conditions for dispensing from pharmacies Under the prescription.

Terms of leave from pharmacies:On prescription

Registration number:LSR-008966/10

Date of registration:31.08.2010

The owner of the registration certificate:BELMEDPREPARATY, RUP BELMEDPREPARATY, RUP Republic of Belarus

Manufacturer: & nbsp

BELMEDPREPARATY, RUP Republic of Belarus

Information update date: & nbsp31.08.2015

Illustrated instructions

Instructions

Timolol (Timolol )